KR20060101456A - Oral Compositions for the Treatment of Cellulite - Google Patents

Abstract

The present invention relates to oral pharmaceutical and cosmetic compositions for the treatment of cellulite containing Vitis vinifera extracts, Centella asiatica triterpenes and dimeric Ginkgo biloba flavonoids, in the free form or complexed with phospholipids.

Description

Oral compositions for the treatment of cellulite

The present invention relates to pharmaceutical and cosmetic compositions containing ingredients of plant origin for the treatment of cellulite.

More specifically, the present invention is grape ( Vitis Pharmaceutical and cosmetic oral compositions for the treatment of cellulite containing active ingredients such as vinifera extracts extract, Ginkgo biloba flavonoid dimers, and Centella asiatica tritelpenes .

According to the invention, the active ingredient is complexed with free form or phospholipids.

Cellulite affects a noticeable increase in the Western population, especially in women, including many adult women of normal body weight who are not obese. Cellulite is associated with a panniculopathy condition, characterized by poor peripheral circulation, oedema, fibrosis and altered fat cell metabolism, and ideal treatment should consider all these aspects. do.

Many pharmaceutical and cosmetic compositions for the treatment of cellulite are readily available on the market: for example of plant origin, ivy, horse-chestmut or kola tree (Centella asiatica) extracts. Caffeine, beta-adrenergic stimulants, methylxanthines, and the like based on these active ingredients. However, nothing really has been proven effective, and often associated with the use of the composition rather than their own use, even with improvements due to diet.

Oral pharmaceutical and / or cosmetic compositions containing a combination of plant-derived active ingredients give the best results for the treatment of cellulite, the accumulation of subcutaneous fat and a marked reduction in the "orange peel" skin of the present invention. Thankfully, it combines different activities of various components, exerts antioedema, antiphosphodiesterasis, vasokinetic activity and promotes collagen production. The compositions of the invention have also been demonstrated to be effective in the treatment of venous insufficiency of the lower limbs.

All active ingredients of the compositions of the invention are known and used in medicaments and / or cosmetics; However, it should be noted that the compositions show a synergistic effect and that the activity of each single activity used is much lower than that of the combination used.

The composition of the present invention is grape ( Vitis vinifera ) standard extract from 10 to 500 mg per unit dose, Ginkgo biloba flavonoid dimer 10 to 500 mg and Centella asiatica asiatica ) 10 to 500 mg or an equivalent amount of the corresponding phospholipid complex.

The free form of components a) -c) is commercially available.

Vitis vinifera) La phospholipid complex (hereinafter referred to as "components a" standard and extract) are described in European Patent No. 275 224. The extract is grapes ( Vitis vinifera ), consisting of polyphenol fractions contained in seeds, containing gallic acid, catechin and epicatechin monomers, dimers, trimers, tetramers, pentamers, hexamers and hepters In free form or in ester form with gallic acid.

In vitro or in vivo experiments showed a high antioxidant capacity of the extract (depending on the experimental model, 10 to 200 times higher than the antioxidant capacity of vitamin E), was able to remove most of the radical species It has a negative effect on the harmful effects. Moreover, the extract could inhibit xanthine-oxidase and chelate Cu ⁺⁺ and Fe ⁺⁺⁺ , thus preventing the enzymatic catalytic production of free radicals in tissues. Finally, grapes ( Vinis vinifera ) extracts inhibit collagenase and other proteases, thereby protecting soft tissues and skin from the harmful effects of proteolytic enzymes upon UV stimulation and during the inflammatory process of the skin; Moreover, the extract has a selective affinity for skin and circulatory structures such as microvessels and capillaries, thus also protecting the circulatory system.

The complex of Ginkgo biloba flavonoid dimer and phospholipid (hereinafter referred to as "component b") is described in European Patent No. 0275005, and the bank ( Ginko biloba ) has the same potency as the free form of flavonoid dimers, but induces greater sustained release of the active substance and better bioavailablity. Ginkgo biloba flavonoid dimers are particularly effective as vascular agents in that they inhibit the release of histamine and cAMP phosphodiesterase from mast cells. In particular, inhibition of cAMP phosphodiesterase increases cAMP levels; Because cAMP activates lipocyte metabolism, these complexes act to lipolyse and improve microvascular perfusion and cutaneous trophism.

Centella asiatica phospholipid complex of the asiatica ) standard extract (hereinafter referred to as "component c") is described in European Patent No. This extract consists of a 4: 3: 3 mixture of three different molecular molecules that show high activity in collagen metabolism; It is composed of asiaticoside, asiatic acid and madecassic acid. These molecules have improved the consumption of fibroblasts of amino acids, mainly L-proline and L-hydroxyproline, and these amino acids have collagen structures in both quantity and quality. Among the most important amino acids. Improved collagen biosynthesis causes rapid replacement of degraded aging fibers with new fibers.

The composition according to the present invention is administered orally in a suitable formulation, and may include liquid preparations (syrups, solutions, suspensions, etc.) or solid preparations (tablets, sugar-coated pills, capsules, chewable tablets, etc.). These formulations can be prepared using suitable excipients by the conventional methods described in "Remington's Pharmaceutical Handbook", Mack Publishing Co., NY, USA.

Examples of compositions according to the invention are described below.

Example 1 : Tablet

Vitis vinifera ) 240 mg phospholipid complex

Bank ( Ginko biloba ) Phospholipid complex of flavonoid dimer 100 mg

Centella asiatica asiatica ) tritelene

Phospholipid Complex 60 mg

Sodium Clos Caramelose 28 mg

Silicon Dioxino 8 mg

Talc 4 mg

Example  2  :

Vitis vinifera extract 150 mg

Bank ( Ginko biloba ) flavonoid dimer 100 mg

Centella asiatica asiatica ) Tritelenes 10 mg

Dicalcium phosphate dihydrate 150 mg

100 mg of microcrystalline cellulose

Clos Caramelose Sodium 28 mg

Silicon dioxide 8 mg

Magnesium Stearate 9 mg

Talc 3 mg

Claims (6)

a) Vitis vinifera ) complexes with standard extracts or their phospholipids; b) complexes with Ginkgo biloba flavonoid dimers or their phospholipids; c) Centella Asiatica asiatica ) or its complex with phospholipids, Oral composition comprising a conventional excipient and a carrier in a mixture. The composition of claim 1, wherein the components of a) -c) are in free form. The composition of claim 1, wherein the components of a) -c) are in complex form with phospholipids. For the preparation of oral pharmaceutical and cosmetic compositions having a cellulite therapeutic action, a) Vitis vinifera ) complexes with standard extracts or their phospholipids; b) complexes with Ginkgo biloba flavonoid dimers or their phospholipids; c) Centella Asiatica asiatica ) or its complex with phospholipids, Use of a combination consisting of: Lower limbs with venous in sufficiency a) Vitis vinifera ) complexes with standard extracts or their phospholipids; b) complexes with Ginkgo biloba flavonoid dimers or their phospholipids; c) Centella Asiatica asiatica ) or its complex with phospholipids, Use of a combination consisting of: Use of the cosmetic composition of claims 1 to 3 having a cellulite therapeutic action.